EP4398867A1 - Use for anti-acne - Google Patents

Use for anti-acne

Info

Publication number
EP4398867A1
EP4398867A1 EP22773457.1A EP22773457A EP4398867A1 EP 4398867 A1 EP4398867 A1 EP 4398867A1 EP 22773457 A EP22773457 A EP 22773457A EP 4398867 A1 EP4398867 A1 EP 4398867A1
Authority
EP
European Patent Office
Prior art keywords
acid
salicylic acid
total
combination
fatty acid
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Pending
Application number
EP22773457.1A
Other languages
German (de)
French (fr)
Inventor
Zhengrong Li
Shuqi Yang
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Unilever Global IP Ltd
Unilever IP Holdings BV
Original Assignee
Unilever Global IP Ltd
Unilever IP Holdings BV
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Unilever Global IP Ltd, Unilever IP Holdings BV filed Critical Unilever Global IP Ltd
Publication of EP4398867A1 publication Critical patent/EP4398867A1/en
Pending legal-status Critical Current

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/33Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • A61K8/36Carboxylic acids; Salts or anhydrides thereof
    • A61K8/361Carboxylic acids having more than seven carbon atoms in an unbroken chain; Salts or anhydrides thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/33Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • A61K8/36Carboxylic acids; Salts or anhydrides thereof
    • A61K8/368Carboxylic acids; Salts or anhydrides thereof with carboxyl groups directly bound to carbon atoms of aromatic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q17/00Barrier preparations; Preparations brought into direct contact with the skin for affording protection against external influences, e.g. sunlight, X-rays or other harmful rays, corrosive materials, bacteria or insect stings
    • A61Q17/005Antimicrobial preparations
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00Preparations for care of the skin

Definitions

  • the present invention relates to new use of a combination of fatty acid and/or salt thereof, and salicylic acid and/or salicylic acid derivative with specific ratio. Such combination is unexpectedly capable of delivering a synergistic anti-acne benefit.
  • Acne also known as Acne vulgaris
  • Acne vulgaris is a common skin condition that affects nearly all adolescents and adults at some point in their lives. It has been observed that acne usually occurs in areas rich in sebaceous glands like the face, neck and back.
  • a bacteria Propionibacterium acnes (P. acnes) has also been implicated in occurrence of acne. It resides in the sebaceous glands. P. acnes uses sebum and by-product from surrounding skin tissue as sources of energy and nutrients, leading to acne or acne vulgaris.
  • the present invention is directed to a combination of (a): Csto C20 fatty acid and/or salt thereof; and (b): salicylic acid and/or salicylic acid derivative, with a weight ratio of total (a) to total (b) being less than 1.7:1 , for use as anti-acne or anti-bacterial agent, wherein the fatty acid is a saturated fatty acid without substitution.
  • the present invention is directed to use of a cosmetic composition for providing anti-acne or anti-bacterial benefit
  • the cosmetic composition comprises a combination of (a): Csto C20 fatty acid and/or salt thereof, and (b): salicylic acid and/or salicylic acid derivative, with a weight ratio of total (a) to total (b) being less than 1.7:1 as anti-acne or anti-bacterial agent, wherein the fatty acid is a saturated fatty acid without substitution.
  • the present invention is directed to a cosmetic composition
  • a cosmetic composition comprising a combination of (a): Csto C20 fatty acid and/or salt thereof, and (b): salicylic acid and/or salicylic acid derivative with a weight ratio of total (a) to total (b) being less than 1.7:1 for providing antiacne or anti-bacterial benefit, wherein the fatty acid is a saturated fatty acid without substitution.
  • the present invention is directed to use of a combination of (a): Csto C20 fatty acid and/or salt thereof, and (b): salicylic acid and/or salicylic acid derivative with a weight ratio of total (a) to total (b) being less than 1.7:1 in a method for providing anti-acne or anti-bacterial benefit, the method comprising topical application of a cosmetic composition comprising said combination, the fatty acid is a saturated fatty acid without substitution.
  • the present invention also provides use of a combination of (a): Csto C20 fatty acid and/or salt thereof, and (b): salicylic acid and/or salicylic acid derivative with a weight ratio of total (a) to total (b) being less than 1.7:1 in the manufacture of medicants for providing anti-acne, or antibacterial function.
  • the present invention also provides use of a combination of (a): Csto C20 fatty acid and/or salt thereof; and (b): salicylic acid and/or salicylic acid derivative, with a weight ratio of total (a) to total (b) being less than 1.7:1 , as anti-acne or anti-bacterial agent.
  • the use is non-therapeutic.
  • the method is non-therapeutic.
  • non-therapeutic typically means for cosmetic purposes and not curative or therapeutic purposes.
  • the fatty acid comprises Cs to C fatty acid, more preferably C10 to C14 fatty acid.
  • the fatty acid has a straight chain with length of 8 to 16, preferably 10 to 14 carbon atoms.
  • the fatty acid is a saturated fatty acid without substitution.
  • the fatty acid comprises lauric acid, stearic acid, myristic acid, oleic acid, linoleic acid, linolenic acid, or a combination thereof. More preferably, the fatty acid comprises lauric acid. Even more preferably, the fatty acid is lauric acid.
  • Salt of fatty acid preferably is sodium salt of fatty acid.
  • (a) is lauric acid and/or salt of lauric acid. More preferably (a) is lauric acid.
  • Salicylic acid derivative as used herein typically comprises ester, and/or salt of salicylic acid.
  • the salicylic acid derivative is ester, and/or salt of salicylic acid. More preferably, the derivative of salicylic acid is salt of salicylic acid.
  • the salicylic acid derivative is selected from acetaminosalol, aspirin, balsalazide, benorylate, calcium acetylsalicylate, diflunisal, fendosal, gentisic acid, glycol salicylate, imidazole salicylate, lysine acetylsalicylate, mesalamine, morpholinesalicylate, 1 -naphthyl salicylate, olsalazine, parsalmide, phenylacetylsalicylate, phenyl salicylate, salicylamide O-acetic acid, salicylsulfuric acid, salsalate, sodium salicylate, sulfasalazine or a combination thereof. More preferably, the salicylic acid derivative is sodium salicylate.
  • (b) is salicylic acid and/or salt of salicylic acid. More preferably, (b) is salicylic acid.
  • the weight ratio of total weight of Csto C20 fatty acid and salt thereof to the total weight of salicylic acid and salicylic acid derivative is 0.1 :1 to 1.7:1 , more preferably 0.2:1 to 1.6:1 , even more preferably 0.4:1 to 1.5:1 , still even more preferably 0.6:1 to 1.4:1 and most preferably 0.7:1 to 1.3:1.
  • the combination is a combination of (a): Csto C20 fatty acid, and (b): salicylic acid or salt of salicylic acid, with a weight ratio of total (a) to total (b) being less than 1.7:1.
  • the weight ratio of Csto C20 fatty acid to the weight of total salicylic acid and salt of salicylic acid is 0.1 :1 to 1.7:1 , more preferably 0.2:1 to 1.6:1 , even more preferably 0.4:1 to 1.5:1 , still even more preferably 0.6:1 to 1.4:1 and most preferably 0.7:1 to 1.3:1.
  • the combination is a combination of (a): lauric acid and/or salt of lauric acid, and (b): salicylic acid and/or salt of salicylic acid, with a weight ratio of total (a) to total (b) being less than 1.7:1.
  • the weight ratio of the total weight of lauric acid and salt of lauric acid to the total weight of salicylic acid and salt of salicylic acid is 0.1 :1 to 1.7:1 , more preferably 0.2:1 to 1.6:1 , even more preferably 0.4:1 to 1.5:1 , still even more preferably 0.6:1 to 1.4:1 and most preferably 0.7:1 to 1.3:1.
  • the combination is a combination of (a): lauric acid, and (b): salicylic acid, with a weight ratio of total (a) to total (b) being less than 1.7:1.
  • the weight ratio of the lauric acid to the salicylic acid is 0.1 :1 to 1.7:1 , more preferably 0.2:1 to 1.6:1 , even more preferably 0.4: 1 to 1 .5: 1 , still even more preferably 0.6: 1 to 1 .4: 1 and most preferably 0.7: 1 to 1 .3: 1.
  • the combination of the present invention typically provides a greater antibacterial, particularly anti-acne benefit in comparison to (a), (b) or a combination of (a) and (b) with a weight ratio of total (a) to total (b) being no less than 1.7:1.
  • the combination of (a): Csto C20 fatty acid and/or salt thereof, and (b): salicylic acid and/or salicylic acid derivative is present in a cosmetic composition.
  • the amount of Csto C20 fatty acid and salt thereof is 0.01 to 8%, more preferably 0.05 to 5%, even more preferably 0.1 to 2% and most preferably 0.2 to 1.2% by weight of the composition.
  • the amount of salicylic acid and salicylic acid derivative is 0.01 to 8%, more preferably 0.05 to 5%, even more preferably 0.1 to 2% and most preferably 0.2 to 1 .2% by weight of the composition.
  • the combination is a combination of (a): Csto C20 fatty acid, and (b): salicylic acid, with a weight ratio of total (a) to total (b) being less than 1.7:1 and the combination is present in a cosmetic composition.
  • the amount of Csto C20 fatty acid is 0.01 to 8%, more preferably 0.05 to 5%, even more preferably 0.1 to 2% and most preferably 0.2 to 1.2% by weight of the composition.
  • the amount of salicylic acid is 0.01 to 8%, more preferably 0.05 to 5%, even more preferably 0.1 to 2% and most preferably 0.2 to 1.2% by weight of the composition.
  • the combination is a combination of (a): lauric acid and/or salt of lauric acid, and (b): salicylic acid and/or salt of salicylic acid, with a weight ratio of total (a) to total (b) being less than 1.7:1 and the combination is present in a cosmetic composition.
  • the total amount of lauric acid and salt of lauric acid is 0.01 to 8%, more preferably 0.05 to 5%, even more preferably 0.1 to 2% and most preferably 0.2 to 1.2% by weight of the composition.
  • the amount of salicylic acid and salt of salicylic acid is 0.01 to 8%, more preferably 0.05 to 5%, even more preferably 0.1 to 2% and most preferably 0.2 to 1.2% by weight of the composition.
  • the combination is a combination of (a): lauric acid, and (b): salicylic acid, with a weight ratio of total (a) to total (b) being less than 1.7:1 and the combination is present in a cosmetic composition.
  • the amount of lauric acid is 0.01 to 8%, more preferably 0.05 to 5%, even more preferably 0.1 to 2% and most preferably 0.2 to 1.2% by weight of the composition.
  • the amount of salicylic acid is 0.01 to 8%, more preferably 0.05 to 5%, even more preferably 0.1 to 2% and most preferably 0.2 to 1.2% by weight of the composition.
  • the cosmetic composition of the present invention typically provides a greater anti-acne and anti-bacterial benefit in comparison to a cosmetic composition that does not contain (a) and (b) with a weight ratio of total (a) to total (b) being less than 1.7:1.
  • the composition preferably comprises a cleansing surfactant. More than one cleansing surfactant may be included in the composition.
  • the cleaning surfactant may be chosen from soap, non-soap anionic, cationic, non-ionic, amphoteric surfactant and mixtures thereof.
  • Many suitable surface-active compounds are available and are fully described in the literature, for example, in "Surface-Active Agents and Detergents", Volumes I and II, by Schwartz, Perry and Berch.
  • the preferred surface-active compounds that can be used are soaps, non-soap anionic, non-ionic surfactant, amphoteric surfactant or a mixture thereof.
  • Suitable non-soap anionic surfactants include linear alkylbenzene sulphonate, primary and secondary alkyl sulphates, particularly Cs to C15 primary alkyl sulphates; alkyl ether sulphates; olefin sulphonates; alkyl xylene sulphonates; dialkyl sulphosuccinates; fatty acid ester sulphonates; or a mixture thereof.
  • Sodium salts are generally preferred.
  • linear alkylbenzene sulphonate particularly linear alkylbenzene sulphonates having an alkyl chain length of from Cs to C15. It is preferred if the level of linear alkylbenzene sulphonate is from 0 wt% to 30 wt%, more preferably from 1 wt% to 25 wt%, most preferably from 2 wt% to 15 wt%, by weight of the total composition.
  • Nonionic surfactants that may be used include the primary and secondary alcohol ethoxylates, especially the Cs to C20 aliphatic alcohols ethoxylated with an average of from 1 to 20 moles of ethylene oxide per mole of alcohol, and more especially the C10 to C15 primary and secondary aliphatic alcohols ethoxylated with an average of from 1 to 10 moles of ethylene oxide per mole of alcohol.
  • Non ethoxylated nonionic surfactants include alkylpolyglycosides, glycerol monoethers, and polyhydroxyamides (glucamide).
  • the level of non-ionic surfactant is from 0 wt% to 30 wt%, preferably from 1 wt% to 25 wt%, most preferably from 2 wt% to 15 wt%, by weight of a fully formulated composition comprising the microcapsules of the invention.
  • Suitable amphoteric surfactants preferably are betaine surfactants.
  • suitable amphoteric surfactants include, but are not limited to, alkyl betaines, alkylamido betaines, alkyl sulfobetaines, alkyl sultaines and alkylamido sultaines; preferably, those having 8 to about 18 carbons in the alkyl and acyl group. It is preferred that the amount of the amphoteric surfactant is 0 to 20 wt%, more preferably from 1 to 10 wt%, by weight of the composition.
  • Cationic surfactants that may be used include quaternary ammonium salts of the general formula R 1 R 2 R 3 R 4 N + X' wherein the R groups are long or short hydrocarbon chains, typically alkyl, hydroxyalkyl or ethoxylated alkyl groups, and X is a counter-ion (for example, compounds in which R 1 is a C8-C22 alkyl group, preferably a Cs-C or C12-C14 alkyl group, R 2 is a methyl group, and R 3 and R 4 , which may be the same or different, are methyl or hydroxyethyl groups); and cationic esters (for example, choline esters).
  • R 1 is a C8-C22 alkyl group, preferably a Cs-C or C12-C14 alkyl group
  • R 2 is a methyl group
  • R 3 and R 4 which may be the same or different, are methyl or hydroxyethyl groups
  • cationic esters
  • Water-soluble skin benefit agents may optionally be formulated into the compositions of the invention.
  • a variety of water-soluble skin benefit agents can be used and the level can be from 0.1 to 50% but preferably from 1 to 30% by weight of the composition. These materials include, but are not limited to, polyhydroxy alcohols.
  • Preferred water-soluble skin benefit agents are glycerin, sorbitol and polyethylene glycol.
  • Water-insoluble skin benefit agents may also be formulated into the compositions as conditioners and moisturizers.
  • conditioners and moisturizers examples include silicone oils; hydrocarbons such as liquid paraffins, petrolatum, microcrystalline wax, and mineral oil; and vegetable triglycerides such as sunflower seed and cottonseed oils.
  • compositions may include thickeners. These may be selected from cellulosics, natural gums and acrylic polymers but not limited by this thickening agent types.
  • cellulosics sodium carboxymethyl cellulose, hydroxyethyl cellulose, hydroxypropyl methylcellulose and combinations thereof.
  • Suitable gums include xanthan, pectin, karaya, agar, alginate gums and combinations thereof.
  • acrylic thickeners are homopolymers and copolymers of acrylic and methacrylic acids including carbomers such as Carbopol 1382, Carbopol 982, llltrez, Aqua SF-1 and Aqua SF-2 available from the Lubrizol Corporation.
  • Amounts of thickener may range from 0.01 to 3% by weight of the active polymer (outside of solvent or water) in the compositions.
  • Preservatives can desirably be incorporated into the compositions of this invention to protect against the growth of potentially harmful microorganisms.
  • Particularly preferred preservatives are phenoxyethanol, methyl paraben, propyl paraben, imidazolidinyl urea, sodium dehydroacetate and benzyl alcohol.
  • the preservatives should be selected having regard for the use of the composition and possible incompatabilities between the preservatives and other ingredients.
  • Preservatives are preferably employed in amounts ranging from 0.01% to 2% by weight of the composition.
  • compositions may include: antimicrobials such as 2-hydroxy-4,2’,4’-trichlorodiphenylether (triclosan), 2,6-dimethyl- 4-hydroxychlorobenzene, and 3,4,4’-trichlorocarbanilide; scrub and exfoliating particles such as polyethylene and silica or alumina; cooling agents such as menthol; skin calming agents such as aloe vera; and colorants.
  • antimicrobials such as 2-hydroxy-4,2’,4’-trichlorodiphenylether (triclosan), 2,6-dimethyl- 4-hydroxychlorobenzene, and 3,4,4’-trichlorocarbanilide
  • scrub and exfoliating particles such as polyethylene and silica or alumina
  • cooling agents such as menthol
  • skin calming agents such as aloe vera
  • compositions of the invention may further include 0.5 to 10% by weight of sequestering agents, such as tetra sodium ethylenediaminetetraacetate (EDTA), EH DP or mixtures; opacifiers and pearlizers such as ethylene glycol distearate, titanium dioxide or Lytron 621 (Styrene/Acrylate copolymer); all of which are useful in enhancing the appearance or properties of the product.
  • sequestering agents such as tetra sodium ethylenediaminetetraacetate (EDTA), EH DP or mixtures
  • opacifiers and pearlizers such as ethylene glycol distearate, titanium dioxide or Lytron 621 (Styrene/Acrylate copolymer); all of which are useful in enhancing the appearance or properties of the product.
  • the composition comprises water in an amount of at least 5% by weight of the composition, more preferably at least 25%, even more preferably 40 to 90% and still even more preferably at least 60 to 85% by weight of the composition.
  • the composition has a viscosity of at least 5 mPa s, more preferably in the range 8 to 10000 mPa s, even more preferably 10 to 1000 mPa s, and most preferably 20 to 200 mPa s, when measured at 20 degrees C at a relatively high shear rate of about 20 s’ 1 .
  • the composition is in the form of fluid.
  • the cosmetic composition refers to a composition suitable for topical application to human skin, preferably is a rinse-off product.
  • rinse-off as used with reference to compositions herein means a composition that is applied to or rubbed on the skin, and then washed off.
  • skin as used herein includes the skin on the face (except eye lids and lips), neck, chest, abdomen, back, arms, under arms, hands, and legs.
  • skin means includes the skin on the face (except eye lids and lips) and under arms, more preferably skin means skin on the face other than lips and eyelids.
  • This example demonstrates the synergy on anti-acne between lauric acid and salicylic acid.
  • Zone of Inhibition of different samples toward Propionibacterium acne (P. acnes) was tested.
  • Samples was prepared according to Table 1. 20 pL of each sample or control sample (aseptic distilled water) were dipped onto identical filter papers and all of these filter papers were dried. Cultures of Propionibacterium acnes were washed and diluted by PBS to suspension with concentration of 1 x10 4 to 9x10 4 cfu/mL. The suspension was evenly smeared on a nutrient agar culture medium plate by aseptic cotton swab. The dried filter papers with samples were closely applied onto the plated with sufficient distances. The plate was covered and cultured at 37 °C for 16 to18 hours. The samples diffuse into the agar are assayed for an ability to produce a zone of inhibition. The diameters of ZOI for different samples were recorded in T able 1. The bigger the ZOI is, the better anti-acne efficiency the sample provides.
  • Sample 1 provided a significant better anti-acne efficiency that any of sample A, B and C. It was surprisingly found that it is capable of providing a synergistic anti-acne benefit when combining lauric acid and salicylic acid with a weight ratio of the lauric acid to the salicylic acid being less than 1.7:1.
  • This example demonstrates a cometic composition containing the combination of lauric acid and the salicylic acid.
  • a skin cleansing composition was prepared according to Table 2 by following standard procedure.

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  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
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Abstract

Disclosed is use of a combination of (a): C8 to C20 fatty acid and/or salt thereof; and (b): salicylic acid and/or salicylic acid derivative, with a weight ratio of total (a) to total (b) being less than 1.7:1, as anti-acne or anti-bacterial agent.

Description

USE FOR ANTI-ACNE
Field of the Invention
The present invention relates to new use of a combination of fatty acid and/or salt thereof, and salicylic acid and/or salicylic acid derivative with specific ratio. Such combination is unexpectedly capable of delivering a synergistic anti-acne benefit.
Background of the Invention
Acne, also known as Acne vulgaris, is a common skin condition that affects nearly all adolescents and adults at some point in their lives. It has been observed that acne usually occurs in areas rich in sebaceous glands like the face, neck and back. A bacteria Propionibacterium acnes (P. acnes) has also been implicated in occurrence of acne. It resides in the sebaceous glands. P. acnes uses sebum and by-product from surrounding skin tissue as sources of energy and nutrients, leading to acne or acne vulgaris.
Although many ways have been developed for treating acne, there is still a need to improve the efficacy of anti-acne. Therefore, the present inventors have developed use of a combination of Csto C20 fatty acid and/or salt thereof, and salicylic acid and/or salicylic acid derivative with a specific weight ratio as anti-acne agent. It was surprisingly found that such combination is capable of providing a synergistic anti-acne benefit.
Summary of the Invention
In a first aspect, the present invention is directed to a combination of (a): Csto C20 fatty acid and/or salt thereof; and (b): salicylic acid and/or salicylic acid derivative, with a weight ratio of total (a) to total (b) being less than 1.7:1 , for use as anti-acne or anti-bacterial agent, wherein the fatty acid is a saturated fatty acid without substitution.
In a second aspect, the present invention is directed to use of a cosmetic composition for providing anti-acne or anti-bacterial benefit, wherein the cosmetic composition comprises a combination of (a): Csto C20 fatty acid and/or salt thereof, and (b): salicylic acid and/or salicylic acid derivative, with a weight ratio of total (a) to total (b) being less than 1.7:1 as anti-acne or anti-bacterial agent, wherein the fatty acid is a saturated fatty acid without substitution. In a third aspect, the present invention is directed to a cosmetic composition comprising a combination of (a): Csto C20 fatty acid and/or salt thereof, and (b): salicylic acid and/or salicylic acid derivative with a weight ratio of total (a) to total (b) being less than 1.7:1 for providing antiacne or anti-bacterial benefit, wherein the fatty acid is a saturated fatty acid without substitution.
In a fourth aspect, the present invention is directed to use of a combination of (a): Csto C20 fatty acid and/or salt thereof, and (b): salicylic acid and/or salicylic acid derivative with a weight ratio of total (a) to total (b) being less than 1.7:1 in a method for providing anti-acne or anti-bacterial benefit, the method comprising topical application of a cosmetic composition comprising said combination, the fatty acid is a saturated fatty acid without substitution.
All other aspects of the present invention will more readily become apparent upon considering the detailed description and examples which follow.
Detailed Description of the Invention
Except in the examples, or where otherwise explicitly indicated, all numbers in this description indicating amounts of material or conditions of reaction, physical properties of materials and/or use may optionally be understood as modified by the word “about”.
All amounts are by weight of the composition, unless otherwise specified.
It should be noted that in specifying any range of values, any particular upper value can be associated with any particular lower value.
For the avoidance of doubt, the word “comprising” is intended to mean “including” but not necessarily “consisting of’ or “composed of”. In other words, the listed steps or options need not be exhaustive.
The disclosure of the invention as found herein is to be considered to cover all embodiments as found in the claims as being multiply dependent upon each other irrespective of the fact that claims may be found without multiple dependency or redundancy.
Where a feature is disclosed with respect to a particular aspect of the invention (for example a composition of the invention), such disclosure is also to be considered to apply to any other aspect of the invention (for example a method of the invention) mutatis mutandis. The present invention also provides use of a combination of (a): Csto C20 fatty acid and/or salt thereof, and (b): salicylic acid and/or salicylic acid derivative with a weight ratio of total (a) to total (b) being less than 1.7:1 in the manufacture of medicants for providing anti-acne, or antibacterial function.
The present invention also provides use of a combination of (a): Csto C20 fatty acid and/or salt thereof; and (b): salicylic acid and/or salicylic acid derivative, with a weight ratio of total (a) to total (b) being less than 1.7:1 , as anti-acne or anti-bacterial agent.
Preferably the use is non-therapeutic. Preferably the method is non-therapeutic. The term non- therapeutic typically means for cosmetic purposes and not curative or therapeutic purposes.
The combination
Preferably, the fatty acid comprises Cs to C fatty acid, more preferably C10 to C14 fatty acid. Preferably the fatty acid has a straight chain with length of 8 to 16, preferably 10 to 14 carbon atoms. The fatty acid is a saturated fatty acid without substitution. Preferably, the fatty acid comprises lauric acid, stearic acid, myristic acid, oleic acid, linoleic acid, linolenic acid, or a combination thereof. More preferably, the fatty acid comprises lauric acid. Even more preferably, the fatty acid is lauric acid. Salt of fatty acid preferably is sodium salt of fatty acid.
Preferably, (a) is lauric acid and/or salt of lauric acid. More preferably (a) is lauric acid.
Salicylic acid derivative as used herein typically comprises ester, and/or salt of salicylic acid. Preferably, the salicylic acid derivative is ester, and/or salt of salicylic acid. More preferably, the derivative of salicylic acid is salt of salicylic acid. Preferably the salicylic acid derivative is selected from acetaminosalol, aspirin, balsalazide, benorylate, calcium acetylsalicylate, diflunisal, fendosal, gentisic acid, glycol salicylate, imidazole salicylate, lysine acetylsalicylate, mesalamine, morpholinesalicylate, 1 -naphthyl salicylate, olsalazine, parsalmide, phenylacetylsalicylate, phenyl salicylate, salicylamide O-acetic acid, salicylsulfuric acid, salsalate, sodium salicylate, sulfasalazine or a combination thereof. More preferably, the salicylic acid derivative is sodium salicylate.
Preferably, (b) is salicylic acid and/or salt of salicylic acid. More preferably, (b) is salicylic acid. Preferably, the weight ratio of total weight of Csto C20 fatty acid and salt thereof to the total weight of salicylic acid and salicylic acid derivative is 0.1 :1 to 1.7:1 , more preferably 0.2:1 to 1.6:1 , even more preferably 0.4:1 to 1.5:1 , still even more preferably 0.6:1 to 1.4:1 and most preferably 0.7:1 to 1.3:1.
Preferably, the combination is a combination of (a): Csto C20 fatty acid, and (b): salicylic acid or salt of salicylic acid, with a weight ratio of total (a) to total (b) being less than 1.7:1. Preferably, the weight ratio of Csto C20 fatty acid to the weight of total salicylic acid and salt of salicylic acid is 0.1 :1 to 1.7:1 , more preferably 0.2:1 to 1.6:1 , even more preferably 0.4:1 to 1.5:1 , still even more preferably 0.6:1 to 1.4:1 and most preferably 0.7:1 to 1.3:1.
Preferably, the combination is a combination of (a): lauric acid and/or salt of lauric acid, and (b): salicylic acid and/or salt of salicylic acid, with a weight ratio of total (a) to total (b) being less than 1.7:1. Preferably, the weight ratio of the total weight of lauric acid and salt of lauric acid to the total weight of salicylic acid and salt of salicylic acid is 0.1 :1 to 1.7:1 , more preferably 0.2:1 to 1.6:1 , even more preferably 0.4:1 to 1.5:1 , still even more preferably 0.6:1 to 1.4:1 and most preferably 0.7:1 to 1.3:1.
Preferably, the combination is a combination of (a): lauric acid, and (b): salicylic acid, with a weight ratio of total (a) to total (b) being less than 1.7:1. Preferably, the weight ratio of the lauric acid to the salicylic acid is 0.1 :1 to 1.7:1 , more preferably 0.2:1 to 1.6:1 , even more preferably 0.4: 1 to 1 .5: 1 , still even more preferably 0.6: 1 to 1 .4: 1 and most preferably 0.7: 1 to 1 .3: 1.
For sake of clarity, the combination of the present invention typically provides a greater antibacterial, particularly anti-acne benefit in comparison to (a), (b) or a combination of (a) and (b) with a weight ratio of total (a) to total (b) being no less than 1.7:1.
Cosmetic composition
Preferably the combination of (a): Csto C20 fatty acid and/or salt thereof, and (b): salicylic acid and/or salicylic acid derivative is present in a cosmetic composition. Preferably, the amount of Csto C20 fatty acid and salt thereof is 0.01 to 8%, more preferably 0.05 to 5%, even more preferably 0.1 to 2% and most preferably 0.2 to 1.2% by weight of the composition. Preferably, the amount of salicylic acid and salicylic acid derivative is 0.01 to 8%, more preferably 0.05 to 5%, even more preferably 0.1 to 2% and most preferably 0.2 to 1 .2% by weight of the composition. Preferably, the combination is a combination of (a): Csto C20 fatty acid, and (b): salicylic acid, with a weight ratio of total (a) to total (b) being less than 1.7:1 and the combination is present in a cosmetic composition. Preferably, the amount of Csto C20 fatty acid is 0.01 to 8%, more preferably 0.05 to 5%, even more preferably 0.1 to 2% and most preferably 0.2 to 1.2% by weight of the composition. Preferably, the amount of salicylic acid is 0.01 to 8%, more preferably 0.05 to 5%, even more preferably 0.1 to 2% and most preferably 0.2 to 1.2% by weight of the composition.
Preferably, the combination is a combination of (a): lauric acid and/or salt of lauric acid, and (b): salicylic acid and/or salt of salicylic acid, with a weight ratio of total (a) to total (b) being less than 1.7:1 and the combination is present in a cosmetic composition. Preferably, the total amount of lauric acid and salt of lauric acid is 0.01 to 8%, more preferably 0.05 to 5%, even more preferably 0.1 to 2% and most preferably 0.2 to 1.2% by weight of the composition. Preferably, the amount of salicylic acid and salt of salicylic acid is 0.01 to 8%, more preferably 0.05 to 5%, even more preferably 0.1 to 2% and most preferably 0.2 to 1.2% by weight of the composition.
Preferably, the combination is a combination of (a): lauric acid, and (b): salicylic acid, with a weight ratio of total (a) to total (b) being less than 1.7:1 and the combination is present in a cosmetic composition. Preferably, the amount of lauric acid is 0.01 to 8%, more preferably 0.05 to 5%, even more preferably 0.1 to 2% and most preferably 0.2 to 1.2% by weight of the composition. Preferably, the amount of salicylic acid is 0.01 to 8%, more preferably 0.05 to 5%, even more preferably 0.1 to 2% and most preferably 0.2 to 1.2% by weight of the composition.
The cosmetic composition of the present invention typically provides a greater anti-acne and anti-bacterial benefit in comparison to a cosmetic composition that does not contain (a) and (b) with a weight ratio of total (a) to total (b) being less than 1.7:1.
The composition preferably comprises a cleansing surfactant. More than one cleansing surfactant may be included in the composition. The cleaning surfactant may be chosen from soap, non-soap anionic, cationic, non-ionic, amphoteric surfactant and mixtures thereof. Many suitable surface-active compounds are available and are fully described in the literature, for example, in "Surface-Active Agents and Detergents", Volumes I and II, by Schwartz, Perry and Berch. The preferred surface-active compounds that can be used are soaps, non-soap anionic, non-ionic surfactant, amphoteric surfactant or a mixture thereof.
Suitable non-soap anionic surfactants include linear alkylbenzene sulphonate, primary and secondary alkyl sulphates, particularly Cs to C15 primary alkyl sulphates; alkyl ether sulphates; olefin sulphonates; alkyl xylene sulphonates; dialkyl sulphosuccinates; fatty acid ester sulphonates; or a mixture thereof. Sodium salts are generally preferred.
Most preferred non-soap anionic surfactant are linear alkylbenzene sulphonate, particularly linear alkylbenzene sulphonates having an alkyl chain length of from Cs to C15. It is preferred if the level of linear alkylbenzene sulphonate is from 0 wt% to 30 wt%, more preferably from 1 wt% to 25 wt%, most preferably from 2 wt% to 15 wt%, by weight of the total composition.
Nonionic surfactants that may be used include the primary and secondary alcohol ethoxylates, especially the Cs to C20 aliphatic alcohols ethoxylated with an average of from 1 to 20 moles of ethylene oxide per mole of alcohol, and more especially the C10 to C15 primary and secondary aliphatic alcohols ethoxylated with an average of from 1 to 10 moles of ethylene oxide per mole of alcohol. Non ethoxylated nonionic surfactants include alkylpolyglycosides, glycerol monoethers, and polyhydroxyamides (glucamide). It is preferred if the level of non-ionic surfactant is from 0 wt% to 30 wt%, preferably from 1 wt% to 25 wt%, most preferably from 2 wt% to 15 wt%, by weight of a fully formulated composition comprising the microcapsules of the invention.
Suitable amphoteric surfactants preferably are betaine surfactants. Examples of suitable amphoteric surfactants include, but are not limited to, alkyl betaines, alkylamido betaines, alkyl sulfobetaines, alkyl sultaines and alkylamido sultaines; preferably, those having 8 to about 18 carbons in the alkyl and acyl group. It is preferred that the amount of the amphoteric surfactant is 0 to 20 wt%, more preferably from 1 to 10 wt%, by weight of the composition.
It is also possible to include certain mono-alkyl cationic surfactants. Cationic surfactants that may be used include quaternary ammonium salts of the general formula R1R2R3R4N+ X' wherein the R groups are long or short hydrocarbon chains, typically alkyl, hydroxyalkyl or ethoxylated alkyl groups, and X is a counter-ion (for example, compounds in which R1 is a C8-C22 alkyl group, preferably a Cs-C or C12-C14 alkyl group, R2 is a methyl group, and R3 and R4, which may be the same or different, are methyl or hydroxyethyl groups); and cationic esters (for example, choline esters).
Water-soluble skin benefit agents may optionally be formulated into the compositions of the invention. A variety of water-soluble skin benefit agents can be used and the level can be from 0.1 to 50% but preferably from 1 to 30% by weight of the composition. These materials include, but are not limited to, polyhydroxy alcohols. Preferred water-soluble skin benefit agents are glycerin, sorbitol and polyethylene glycol.
Water-insoluble skin benefit agents may also be formulated into the compositions as conditioners and moisturizers. Examples include silicone oils; hydrocarbons such as liquid paraffins, petrolatum, microcrystalline wax, and mineral oil; and vegetable triglycerides such as sunflower seed and cottonseed oils.
Some compositions may include thickeners. These may be selected from cellulosics, natural gums and acrylic polymers but not limited by this thickening agent types. Among the cellulosics are sodium carboxymethyl cellulose, hydroxyethyl cellulose, hydroxypropyl methylcellulose and combinations thereof. Suitable gums include xanthan, pectin, karaya, agar, alginate gums and combinations thereof. Among the acrylic thickeners are homopolymers and copolymers of acrylic and methacrylic acids including carbomers such as Carbopol 1382, Carbopol 982, llltrez, Aqua SF-1 and Aqua SF-2 available from the Lubrizol Corporation. Amounts of thickener may range from 0.01 to 3% by weight of the active polymer (outside of solvent or water) in the compositions.
Preservatives can desirably be incorporated into the compositions of this invention to protect against the growth of potentially harmful microorganisms. Particularly preferred preservatives are phenoxyethanol, methyl paraben, propyl paraben, imidazolidinyl urea, sodium dehydroacetate and benzyl alcohol. The preservatives should be selected having regard for the use of the composition and possible incompatabilities between the preservatives and other ingredients. Preservatives are preferably employed in amounts ranging from 0.01% to 2% by weight of the composition.
A variety of other optional materials may be formulated into the compositions. These may include: antimicrobials such as 2-hydroxy-4,2’,4’-trichlorodiphenylether (triclosan), 2,6-dimethyl- 4-hydroxychlorobenzene, and 3,4,4’-trichlorocarbanilide; scrub and exfoliating particles such as polyethylene and silica or alumina; cooling agents such as menthol; skin calming agents such as aloe vera; and colorants.
In addition, the compositions of the invention may further include 0.5 to 10% by weight of sequestering agents, such as tetra sodium ethylenediaminetetraacetate (EDTA), EH DP or mixtures; opacifiers and pearlizers such as ethylene glycol distearate, titanium dioxide or Lytron 621 (Styrene/Acrylate copolymer); all of which are useful in enhancing the appearance or properties of the product.
Preferably the composition comprises water in an amount of at least 5% by weight of the composition, more preferably at least 25%, even more preferably 40 to 90% and still even more preferably at least 60 to 85% by weight of the composition.
Preferably, the composition has a viscosity of at least 5 mPa s, more preferably in the range 8 to 10000 mPa s, even more preferably 10 to 1000 mPa s, and most preferably 20 to 200 mPa s, when measured at 20 degrees C at a relatively high shear rate of about 20 s’1.
Preferably, the composition is in the form of fluid.
The cosmetic composition refers to a composition suitable for topical application to human skin, preferably is a rinse-off product. The term "rinse-off" as used with reference to compositions herein means a composition that is applied to or rubbed on the skin, and then washed off. The term "skin" as used herein includes the skin on the face (except eye lids and lips), neck, chest, abdomen, back, arms, under arms, hands, and legs. Preferably “skin” means includes the skin on the face (except eye lids and lips) and under arms, more preferably skin means skin on the face other than lips and eyelids.
The following examples are provided to facilitate an understanding of the invention. The examples are not intended to limit the scope of the claims.
Examples
Example 1
This example demonstrates the synergy on anti-acne between lauric acid and salicylic acid.
Table 1
*Significantly better than any of A, B, C (p<0.05)
Zone of Inhibition (ZOI) of different samples toward Propionibacterium acne (P. acnes) was tested. Samples was prepared according to Table 1. 20 pL of each sample or control sample (aseptic distilled water) were dipped onto identical filter papers and all of these filter papers were dried. Cultures of Propionibacterium acnes were washed and diluted by PBS to suspension with concentration of 1 x104to 9x104 cfu/mL. The suspension was evenly smeared on a nutrient agar culture medium plate by aseptic cotton swab. The dried filter papers with samples were closely applied onto the plated with sufficient distances. The plate was covered and cultured at 37 °C for 16 to18 hours. The samples diffuse into the agar are assayed for an ability to produce a zone of inhibition. The diameters of ZOI for different samples were recorded in T able 1. The bigger the ZOI is, the better anti-acne efficiency the sample provides.
It is evident from Table 1 that Sample 1 provided a significant better anti-acne efficiency that any of sample A, B and C. It was surprisingly found that it is capable of providing a synergistic anti-acne benefit when combining lauric acid and salicylic acid with a weight ratio of the lauric acid to the salicylic acid being less than 1.7:1.
Example 2
This example demonstrates a cometic composition containing the combination of lauric acid and the salicylic acid.
A skin cleansing composition was prepared according to Table 2 by following standard procedure.
Table 2
Example 3
This example demonstrates there is no synergy on anti-acne benefit between oleic acid and salicylic acid.
The experiments were conducted in a similar manner as described in Example except that: i) oleic acid was employed to replace lauric acid; ii) the concentration of Propionibacterium acnes for testing ZOI was 1 x108to 9x108 cfu/mL iii) The plate was covered and cultured at 37 °C for 46 to 48 hours. Table 3 shows the test results.
Table 3
*significant lower than E (p<0.05)
As shown in Table 3, there is no synergistic anti-acne efficiency when combining oleic acid and salicylic acid.

Claims

Claims
1. A combination of (a): Csto C20 fatty acid and/or salt thereof; and (b): salicylic acid and/or salicylic acid derivative, with a weight ratio of total (a) to total (b) being less than 1.7:1 , for use as anti-acne or anti-bacterial agent, wherein the fatty acid is a saturated fatty acid without substitution.
2. The combination according to claim 1 wherein the fatty acid has a straight chain with length of 10 to 14 carbon atoms, preferably the fatty acid is lauric acid.
3. The combination according to claim 1 or 2 wherein (b) is salicylic acid and/or salt of salicylic acid, preferably (b) is salicylic acid.
4. The combination according to any one of the preceding claims wherein the weight ratio of total weight of Csto C20 fatty acid and salt thereof to the total weight of salicylic acid and salicylic acid derivative is 0.2:1 to 1.6:1 , preferably 0.7:1 to 1.3:1.
5. The combination according to any one of the preceding claims wherein the combination is a combination of (a): lauric acid and/or salt of lauric acid, and (b): salicylic acid and/or salt of salicylic acid, with a weight ratio of total (a) to total (b) being less than 1.7:1.
6. The combination according to claim 5 wherein the weight ratio of the total weight of lauric acid and salt of lauric acid to the total weight of salicylic acid and salt of salicylic acid is 0.2:1 to 1.6:1 , preferably 0.7:1 to 1.3:1.
7. The combination according to any one of the preceding claims wherein the combination is a combination of (a): lauric acid, and (b): salicylic acid, with a weight ratio of total (a) to total (b) being less than 1.7:1.
8. The combination according to claim 7 wherein the weight ratio of the lauric acid to the salicylic acid is 0.2:1 to 1.6:1, preferably 0.7:1 to 1.3:1.
9. Non-therapeutical use of the combination according to any one of the preceding claims as anti-acne or anti-bacterial agent in a cosmetic composition, wherein the fatty acid is a saturated fatty acid without substitution. Use of a cosmetic composition for providing anti-acne or anti-bacterial benefit, wherein the cosmetic composition comprises a combination of (a): Csto C20 fatty acid and/or salt thereof, and (b): salicylic acid and/or salicylic acid derivative, with a weight ratio of total (a) to total (b) being less than 1.7:1 as anti-acne or anti-bacterial agent, wherein the fatty acid is a saturated fatty acid without substitution. A cosmetic composition comprising a combination of (a): Csto C20 fatty acid and/or salt thereof, and (b): salicylic acid and/or salicylic acid derivative with a weight ratio of total (a) to total (b) being less than 1.7:1 for providing anti-acne or anti-bacterial benefit, wherein the fatty acid is a saturated fatty acid without substitution. Use of a combination of (a): Csto C20 fatty acid and/or salt thereof, and (b): salicylic acid and/or salicylic acid derivative with a weight ratio of total (a) to total (b) being less than 1.7:1 in a method for providing anti-acne or anti-bacterial benefit, the method comprising topical application of a cosmetic composition comprising said combination, wherein the fatty acid is a saturated fatty acid without substitution. The use, composition or method according to any one of the preceding claims 9 to 12 wherein the total amount of Csto C20 fatty acid and salt thereof is 0.01 to 8%, preferably 0.1 to 2% and by weight of the composition and the total amount of salicylic acid and salicylic acid derivative is 0.01 to 8% preferably 0.1 to 2% by weight of the composition. The use, composition or method according to any one of the preceding claims 9 to 13 wherein the total amount of lauric acid and salt of lauric acid, is 0.01 to 8%, preferably 0.1 to 2% and by weight of the composition and the total amount of salicylic acid and salicylic acid derivative is 0.01 to 8% preferably 0.1 to 2% by weight of the composition. The use, composition or method according to any one of the preceding claims 9 to 14 wherein the amount of lauric acid is 0.01 to 8%, preferably 0.1 to 2% and by weight of the composition and the amount of salicylic acid is 0.01 to 8% preferably 0.1 to 2% by weight of the composition.
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US6270752B1 (en) * 1997-10-17 2001-08-07 Giancarlo Verona Cosmetic formulations for the prevention and therapy of hair loss

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AU619256B2 (en) * 1988-03-03 1992-01-23 Connetics Australia Pty Ltd Acne treatment
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CN108992389A (en) * 2018-10-23 2018-12-14 江苏朗沁科技有限公司 A kind of light spot dressing of anti-acne
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US6270752B1 (en) * 1997-10-17 2001-08-07 Giancarlo Verona Cosmetic formulations for the prevention and therapy of hair loss

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